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Avutometinib

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Chemical compound

Pharmaceutical compound

Avutometinib
Clinical data

Skeletal formula andball-and-stick model of avutometinib
Other names	RO-5126766; CH-5126766; CKI-27; R-7304; RG-7304
Pharmacokinetic data
Eliminationhalf-life	60 h (45.8–93.7 h)
Identifiers
IUPAC name 3-[[3-fluoro-2-(methylsulfamoylamino)pyridin-4-yl]methyl]-4-methyl-7-pyrimidin-2-yloxychromen-2-one
CAS Number	946128-88-7
PubChemCID	16719221
DrugBank	DB15254
ChemSpider	17623621
UNII	D0D4252V97
KEGG	D12515
ChEBI	CHEBI:78825
ChEMBL	ChEMBL3264002
PDB ligand	CHU (PDBe,RCSB PDB)
Chemical and physical data
Formula	C₂₁H₁₈FN₅O₅S
Molar mass	471.46 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES CC1=C(C(=O)OC2=C1C=CC(=C2)OC3=NC=CC=N3)CC4=C(C(=NC=C4)NS(=O)(=O)NC)F
InChI InChI=1S/C21H18FN5O5S/c1-12-15-5-4-14(31-21-25-7-3-8-26-21)11-17(15)32-20(28)16(12)10-13-6-9-24-19(18(13)22)27-33(29,30)23-2/h3-9,11,23H,10H2,1-2H3,(H,24,27) Key:LMMJFBMMJUMSJS-UHFFFAOYSA-N

Avutometinib (INN; codenamedRO-5126766,CH-5126766,CKI-27,R-7304,RG-7304, andVS-6766 at various stages of its development) is aninhibitor ofRas-Raf-MEK-ERK signaling being developed as a potential treatment forcancer.

It was discovered byChugai Pharmaceutical Co. (a subsidiary ofRoche) throughderivatization of ahit compound identified byhigh-throughput screening.^[1] It was licensed byVerastem Oncology in 2020 for clinical trials.^[2]^[3]

The co-packaged medicationavutometinib/defactinib was approved for medical use in the United States in May 2025.^[4]^[5]

References

[edit]

^Ishii N, Harada N, Joseph EW, Ohara K, Miura T, Sakamoto H, Matsuda Y, Tomii Y, Tachibana-Kondo Y, Iikura H, Aoki T, Shimma N, Arisawa M, Sowa Y, Poulikakos PI, Rosen N, Aoki Y, Sakai T (July 2013)."Enhanced inhibition of ERK signaling by a novel allosteric MEK inhibitor, CH5126766, that suppresses feedback reactivation of RAF activity".Cancer Res.73 (13):4050–4060.doi:10.1158/0008-5472.CAN-12-3937.PMC 4115369.PMID 23667175.
^Adams, Ben (8 January 2020)."Verastem pens KRAS-focused drug licensing deal with Chugai". Fierce Biotech. Retrieved5 June 2022.
^"Drug Profile: Avutometinib"(PDF).AdisInsight. 23 May 2022. Retrieved5 June 2022.
^"FDA grants accelerated approval to the combination of avutometinib and defactinib for KRAS-mutated recurrent low-grade serous ovarian cancer".U.S.Food and Drug Administration. 8 May 2025. Archived fromthe original on 8 May 2025. Retrieved16 May 2025. This article incorporates text from this source, which is in thepublic domain.
^"FDA Approves the Avmapki Fakzynja Combination Therapy as the First-Ever Treatment for Adult Patients with KRAS-mutated Recurrent Low-Grade Serous Ovarian Cancer".Verastem (Press release). Retrieved16 May 2025.

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